From the Guidelines
Patients taking ezetimibe for hyperlipidemia should be monitored for liver function with baseline hepatic transaminases obtained before initiation of ezetimibe, and as clinically indicated when coadministered with a statin 1.
Monitoring Parameters
- Liver function tests: Alanine transaminase (ALT) levels should be assessed at initiation of therapy and periodically thereafter, typically every 3-6 months for the first year.
- Lipid profiles: Should be evaluated at baseline, 4-6 weeks after initiation, and every 3-6 months thereafter to assess efficacy, as recommended for patients on statin therapy or other lipid-lowering therapy 1.
- Signs and symptoms of myopathy: Particularly when co-administered with statins, and creatine kinase (CK) levels should be assessed if muscle symptoms occur.
Additional Considerations
- Patients should be monitored for adverse effects, and the potential benefits and risks of ezetimibe should be reassessed if any adverse effects occur.
- The dose of ezetimibe may need to be adjusted based on the patient's response to therapy and the presence of any adverse effects.
- It is reasonable to use ezetimibe in addition to statin therapy in patients with diabetes and high cardiovascular risk, as it may help to reduce LDL cholesterol levels by 50% or more 1.
From the FDA Drug Label
The incidence of consecutive increased transaminases (≥3 X ULN) was higher in patients receiving ezetimibe tablets administered with statins (1.3%) than in patients treated with statins alone (0. 4%). Incidence rates for clinically important elevations (≥3 X ULN, consecutive) in hepatic transaminase levels were 4.5% and 2.7% for fenofibrate monotherapy (n=188) and ezetimibe tablets coadministered with fenofibrate (n=183), respectively, adjusted for treatment exposure. Table 3 includes a list of drugs with clinically important drug interactions when administered concomitantly with ezetimibe tablets and instructions for preventing or managing them Monitor cyclosporine concentrations in patients receiving ezetimibe tablets and cyclosporine. If cholelithiasis is suspected in a patient receiving ezetimibe tablets and fenofibrate, gallbladder studies are indicated, and alternative lipid-lowering therapy should be considered.
Key Monitoring Parameters:
- Liver function tests: Monitor for increased transaminases (≥3 X ULN) when co-administered with statins or fenofibrate 2
- Cyclosporine concentrations: Monitor in patients receiving ezetimibe tablets and cyclosporine 2
- Gallbladder function: Monitor for cholelithiasis in patients receiving ezetimibe tablets and fenofibrate 2
From the Research
Monitoring Parameters
When a patient is taking ezetimibe for hyperlipidemia, the following parameters should be monitored:
- Liver function tests, as ezetimibe can cause elevations in liver enzymes 3, 4
- Creatine kinase levels, as ezetimibe can cause muscle damage 3
- Lipid profiles, including low-density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C), and triglycerides, to assess the efficacy of treatment 3, 4, 5, 6, 7
- Adverse events, such as treatment-related adverse events, discontinuations due to adverse events, and serious adverse events 3
Safety and Tolerability
Ezetimibe has been shown to be well tolerated and safe when coadministered with statins 3, 4, 5, 6, 7. However, patients should be monitored for potential adverse events, such as:
- Elevations in liver function tests 3, 4
- Muscle damage, as indicated by elevated creatine kinase levels 3
- Other adverse events, such as gastrointestinal symptoms or allergic reactions 3, 4, 5, 6, 7
Efficacy
Ezetimibe has been shown to be effective in reducing LDL-C levels when coadministered with statins 3, 4, 5, 6, 7. The efficacy of ezetimibe can be assessed by monitoring: